Plasma Protein Binding as an Optimizable Parameter for In Vivo Efficacy

Plasma protein is crucial for understanding pharmacokinetics, pharmacodynamics, and safety, yet it is often not recommended as a primary parameter for optimization in drug design. This study challenges this view by revisiting established pharmacokinetic models to elucidate a bidirectional strategy for clearance-dependent optimization of plasma protein binding. The analysis shows that strategically modulating plasma protein binding can enhance drug efficacy and safety, supporting its consideration as a key factor in the drug design process.